Normal bones are living tissues undergoing constant resorption and redeposition of calcium, with the net effect of maintenance of a constant mineral balance. The dual process is commonly called "bone turnover". In normal growing bones, the mineral deposition is in equilibrium with the mineral resorption, whereas in certain pathological conditions, bone resorption exceeds bone deposition, for instance due to malignancy or primary hyperparathyroidism, or in osteoporosis. In other pathological conditions the calcium deposition may take place in undesirable amounts and areas leading to e.g. heterotopic calcification, osteoarthritis, kidney or bladder stones, atherosclerosis, and Paget's disease which is a combination of an abnormal high bone resorption followed by an abnormal calcium deposition.
Alendronate, 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium trihydrate, is an agent for combating bone resorption in bone diseases including osteoporosis and is described as a composition, method of use and synthesis along with other pharmaceutically acceptable salts in U.S. Pat. Nos. 4,922,007 and 5,019,651 (both assigned to Merck).
There are situations where e.g., an aging female patient is undergoing alendronate therapy for osteoporosis (i.e. rarefaction of bone) or is considered to be at risk for developing osteoporosis and at the same time experiences difficulty in swallowing.
However, alendronate currently is administered orally to all patients as a tablet. The availability of only a solid oral dosage form is a disadvantage for some patients who are unable to readily swallow tablets. Furthermore, these patients may comprise a significant percentage of the alendronate patient population, since the drug is also intended for the aging female patient population.
What is desired in these cases is an effective therapy to optimally treat this aging female patient population with an improved oral formulation to overcome the problem of difficulty in swallowing.